2. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling
  3. GSK-3 Tau Protein
  4. GSK3β-IN-4

GSK3β-IN-4 是一种选择性、强效、具有口服活性且能穿透血脑屏障的 ATP 竞争性 GSK3β 抑制剂，其 IC50 值为 0.37 nM。GSK3β-IN-4 对 GSK3α 的 IC50 值为 2.75 nM，SI 为 7.4。GSK3β-IN-4 通过抑制 GSK3β 来减少 Ser396 位点的 tau 蛋白磷酸化，并能改善阿尔茨海默病模型中的认知缺陷。GSK3β-IN-4 可用于阿尔茨海默病的研究。

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GSK3β-IN-4

GSK3β-IN-4 Chemical Structure

CAS No. : 3083425-61-7

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GSK3β-IN-4 相关抗体

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查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC50 of 0.37 nM. GSK3β-IN-4 shows an IC50 of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.37 nM (IC50)

GSK-3α

2.75 nM (IC50)

体外研究
(In Vitro)

GSK3β-IN-4 (Compound 39a) 在 Tau (P301L) 293T 细胞中显著抑制 Ser396 位点的 Tau 磷酸化，其 EC50 值为 0.06 μM，且细胞毒性低 (IC50 = 80.75 μM)[1] 。
GSK3β-IN-4 在 1 × Km、10 × Km、100 × Km ATP 浓度下，对 GSK3β 的 IC50 值分别为 1.27 nM、7.14 nM、77.8 nM，呈 ATP 竞争性抑制模式[1] 。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GSK3β-IN-4 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 2.5 mg/kg i.v. T1/2 0.39 h
Mice[1] 2.5 mg/kg i.v. Cmax 1.09 μg/mL
Mice[1] 2.5 mg/kg i.v. AUC0-t 0.63 μg·h/mL
Mice[1] 2.5 mg/kg i.v. AUC0-∞ 0.63 μg·h/mL
Mice[1] 2.5 mg/kg i.v. CL 3.99 L/h/kg
Mice[1] 2.5 mg/kg i.v. Vss 2.24 L/kg
Mice[1] 2.5 mg/kg i.v. Tmax 0.08 h
Mice[1] 25 mg/kg p.o. T1/2 1.78 h
Mice[1] 25 mg/kg p.o. Cmax 1.24 μg/mL
Mice[1] 25 mg/kg p.o. AUC0-t 1.02 μg·h/mL
Mice[1] 25 mg/kg p.o. AUC0-∞ 1.069 μg·h/mL
Mice[1] 25 mg/kg p.o. F 16.2 %
Mice[1] 25 mg/kg p.o. Tmax 0.25 h
体内研究
(In Vivo)

GSK3β-IN-4 (Compound 39a) (1000 mg/kg, 口服, 单次给药) 对 C57BL/6J 小鼠无致死性，14 天内体重正常增长，无行为异常，主要脏器无病理损伤[1]。
GSK3β-IN-4 (5-25 mg/kg, 口服, 每日 1 次，连续 14 天) 在 Okadaic acid (HY-N6785) 诱导的阿尔茨海默病小鼠模型中改善认知缺陷和 Tau Ser396 磷酸化水平[1]。
GSK3β-IN-4 (5 mg/kg, 口服, 每日 1 次，连续 60 天) 改善 6 月龄 3×Tg-AD 小鼠的空间学习记忆障碍，降低海马体 CA3 区 Tau Ser396 磷酸化水平，效果与 Donepezil (HY-14566) (5 mg/kg) 相当，且无运动功能影响[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (Okadaic acid-induced model of Alzheimer's disease)[1]
Dosage: 5 mg/kg, 25 mg/kg
Administration: Orally administration
Result: Reduced tau phosphorylation (pS396) in the hippocampus and temporal.
Reduced escape latency and improved spatial memory retention, as evidenced by increased time spent in the target quadrant and higher platform-crossing frequency.
Did not cause locomotor dysfunction.
Animal Model: 3×Tg-AD mice (transgenic model of Alzheimer's disease)[1]
Dosage: 5 mg/kg
Administration: Orally administration
Result: Improved spatial learning and memory deficits.
Reduced escape latency during hidden platform trials and increased time spent in the target quadrant during probe tests.
Revealed a reduction in pS396 tau levels in the hippocampal CA3 region.
分子量

426.51

Formula

C26H26N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GSK3β-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

GSK3β-IN-43083425-61-7GSK-3Tau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3GSK3βTau phosphorylationSer396293TOkadaic acidTg-ADInhibitorinhibitorinhibit

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